PROTAC NTRK1 degrader-1
PROTAC NTRK1 degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). PROTAC NTRK1 degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1. PROTAC NTRK1 degrader-1 can be used for the research of solid tumors.
(Pink: NTRK1 ligand (HY-185545); Blue: Cereblon ligand (HY-W1115186); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2922274-35-7
- Formula: C38H35FN10O6
- Molecular Weight:746.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
NTRK degrader-1 (compound 5b) (6 h) degrades wild-type NTRK1, NTRK1G595R, NTRK1G667C, and NTRK1F598L in 293 T cells at 6 h, with the IP (inflection point) values of 0.2 nM, 1 nM, 2 nM, and 0.2 nM, respectively[1].
NTRK degrader-1 inhibits wild-type NTRK1, NTRK1G595R, NTRK1G667C, and NTRK1F598L with IC50 values of 4 nM, 2 nM, 5 nM and <0.5 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | T1/2 | Vss |
|---|---|---|---|---|---|
| Mice[1] | 0.5 mg/kg | i.v. | 62 mL/mg/kg | 1.6 h | 3.1 L/kg |
Chemical Information
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CAS No. 2922274-35-7
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Molecular Weight 746.75
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Formula C38H35FN10O6
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SMILES
O=C1NC(C=CC(C(NCC(N2CCN(C3=CC=C(NC4CCC(NC4=O)=O)C=C3)CC2)=O)=O)=C5)=C5OC(C=CC(F)=C6)=C6CNC7=NC8=C1C=NN8C=C7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC NTRK1 degrader-1 Related Classifications
HY-181052 Related Classifications
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